Synergistic effects, augmenting antimicrobal effects of lipids

Abstract

This invention relates to novel synergy, where the antimicrobial effects of microbicidal lipids are augmented with minor amounts of ethanol, in particular to augment the microbicidal effects for preventing infection in the nasal, ocular, otal, pharynx, larynx, sinuses, oral cavity, vaginal or dermal surface of a mammal by virus, pathogenic bacteria or fungi.

1 . A method of treatment of a disease or condition in a mammal, selected from infection in the nasal cavity, ocular region, inner ear, pharynx, larynx, sinuses, oral cavity, vaginal or dermal surface of a mammal, caused by virus, pathogenic bacteria or fungi, comprising administering to said mammal a formulation comprising in the range from about 0.01% to about 5% of an antimicrobially active lipid, and ethanol in a concentration in the range from about 0.1% to about 4%, and a physiologically acceptable vehicle. 
     
     
         2 . The method according to  claim 1 , wherein said antimicrobially active lipid is selected from the group consisting of glycerol monocaprate, glycerol monocaprylate, glycerol monolaurate, propylene glycol monocaprate, propylene glycol monocaprylate, propylene glycol monolaurate, glycerol dicaprin, glycerol dicaprylate, glycerol dilaurate, glycerol tricaprin, glycerol tricaprylate, glycerol trilaurate, octylglycerol, monomyristin, monopalmitolein, monoolein, propylene glycol monocaprylate, propylene glycol monolaurate, and any combination thereof. 
     
     
         3 . The method according to  claim 1 , wherein said formulation comprises ethanol in the range from about 0.2% to about 3%. 
     
     
         4 . The method according to  claim 1 , wherein said antimicrobially active lipid is present in said formulation in a concentration in the range from about 0.05% to about 2%. 
     
     
         5 . The method according to  claim 1 , wherein said formulation is in a form selected from the group consisting of solution, ointment, spray, aerosol, mist, drops, creme, gel, suppository, and vagitory. 
     
     
         6 . The method according to  claim 1 , wherein said formulation further comprises methoxy-polyethylene glycol. 
     
     
         7 . The method according to  claim 6 , wherein said methoxypolyethylene glycol is represented by formula I:
   CH 3 —(O—CH 2 —CH 2 ) n —H  (I)
   wherein n is an integer in the range from 1 to 25.   
     
     
         8 . The method according to  claim 6 , wherein said methoxypolyethylene glycol in said formulation is in a concentration within the range from about 0.1% to about 60%. 
     
     
         9 . The method according to  claim 1 , wherein said formulation further comprises one or more excipient selected from the group consisting of absorption promoters, water absorbing polymers, microspheres, oils, emulsions, liposomes, substances that inhibit enzymatic degradation, alcohols, organic solvents, water, surfactants, hydrophobic agents, pH-controlling agents, preservatives and osmotic pressure controlling agents, cyclodextrins and propellants or mixtures thereof. 
     
     
         10 . The method according to  claim 15 , wherein said formulation further comprises a substance selected from polyethylene glycol, a buffer, a spermicide such as nonoxynol-9, a chelating agent, including EDTA. 
     
     
         11 . The method according to  claim 1 , comprising administering said formulation via an administration route selected from topical administration to skin, administration to oral cavity, administration to nasal mucosa, ocular administration, otal administration, administration pharynx, administration larynx, administration sinuses, vaginal administration, rectal administration, and topical administration to nails. 
     
     
         12 . The method according to  claim 1 , comprising administering said formulation in a dosage unit of less than 10 mL. 
     
     
         13 . The method according to  claim 1 , comprising administering said formulation in a dosage unit of less than 1 mL. 
     
     
         14 . The method according to  claim 1 , wherein said mammal is a human. 
     
     
         15 . A method to augment the microbicidal or antimicrobial effects of antimicrobially active lipid in a pharmaceutical formulation, comprising admixing in the formulation ethanol in a concentration within the range of 0.1-4%. 
     
     
         16 . The method according to  claim 15 , wherein said ethanol is in a concentration in the range from about 0.2 to about 3%. 
     
     
         17 . The method according to  claim 15 , wherein the antimicrobially active lipid is in a concentration in the range from about 0.1% to about 1%.